A simple Schiff base, N-(pyridine-4-yl-methylene) quinuclidine-3-amine was synthesized from 3-aminoquinuclidine and 4-pyridine carboxaldehyde. The physico-chemical properties of the synthesized compound were studied. Molecular docking study was carried out and the quinuclidine derivative was evaluated for its in vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum str...

Results from in vitro experiments, using the hypogastric nerve--vas deferens preparation, and the phrenic nerve--hemidiaphragm preparation of the guineapig, have been used to determine the separation between the neuromuscular and ganglionic blocking effects of atracurium and tubocurarine. Regression lines were used to calculate the concentrations of each drug (99% confidence limits) which would...

Inositol phosphate glycan pseudotetrasaccharides consisting of man-(alpha1-6)-man-(alpha1-4)-glcN-(alpha,beta1-6)-myo-inositol-1,2-cyclic phosphate possessing a sulfate group at either O-6 (compounds 3alpha,beta) or O-2 (compounds 4alpha,beta) of the terminal mannose have been prepared. Compound 4alpha was able to stimulate lipogenesis in native rat adipocytes to 78% of the maximal insulin resp...

The quantitative structure-activity relationships (QSARs) for polychlorinated biphenyl (PCB) congeners have been determined by comparing the EC50 values for three in vitro test systems, namely, aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin O-deethylase (EROD) induction in rat hepatoma H-4-II-E cells and competitive binding avidities to the rat cytosolic receptor protein (using 2,3,7,8-...

Recent advances in Immuno-Oncology (IO) have shown that the immune system can be activated to induce long term durable anti-tumor responses. For IO drug development, immune activation is typically explored using rat surrogate antibodies in immunocompetent mouse models. While these models can be used to show efficacy in vivo, the development of anti-drug immune responses to experimental protein-...

In vitro antioxidant activities of three sweet dihydrochalcone glucosides from the leaves of Lithocarpus pachyphyllus (Kurz) Rehd. (Fagaceae), trilobatin 2"-acetate (1), phloridzin (2) and trilobatin (3), were investigated. The IC50 (50% inhibitory concentration) values for compounds 1-3 of lipid peroxidation in rat liver homogenate were 261, 28, 88 microM, respectively. Compounds 1-3 increased...

The toxicity to Chlorella vulgaris, expressed as log(1/EC50), of two sets of aromatic compounds has been examined. For the first set, which consists of 13 monoand di-substituted nitrobenzenes, it was found that oneor two-descriptor models provide useful correlations. A six-descriptor regression model for the log(1/EC50) values of a larger set that consists of 49 aromatic compounds has also been...

Objective(s): In the present study, the effect of tissue incubation with propranolol on functional antagonism of Zataria multiflora Boiss (Z. multiflora) at muscarinic receptors of tracheal smooth muscle was examined.  Materials and Methods: The effects of three concentrations of aqueous-ethanolic extract, 10 nM atropine, and saline on muscarinic receptors were tested on incubated tracheal smoo...

The stimulatory effect of the extract of Portulaca oleracea (P. olerace) on β-adrenoceptor of tracheal smooth muscle was examined. To examine β-adrenoceptor stimulatory effect, concentration response curve to isoprenaline was obtained in pre-contracted tracheal smooth muscle in the presence of three concentrations of aqueous-ethanolic extract, propranolol and saline. Values of EC50 (the effecti...

Four conformationally restricted analogues of pentamidine were prepared. Then, different concentrations (0.039, 0.078, 0.156, 0.312 and 0.625 mg/mL) of each compound and two positive controls (amphotericin B and pentamidine, 0.625 mg/mL), one negative control (culture medium) and one solvent control (DMSO) were prepared and placed in 24-well plates containing 50000 parasite per well. Promastigo...